Inside Back Cover: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. Int. Ed. 30/2015) | Zendy

Frett Brendan | Zendy; Carlomagno Francesca | Zendy; Moccia Maria Luisa | Zendy; Brescia Annalisa | Zendy; Federico Giorgia | Zendy; De Falco Valentina | Zendy; Admire Brittany | Zendy; Chen Zhongzhu | Zendy; Qi Wenqing | Zendy; Santoro Massimo | Zendy; Li Hongyu | Zendy

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Inside Back Cover: Fragment‐Based Discovery of a Dual pan‐RET/VEGFR2 Kinase Inhibitor Optimized for Single‐Agent Polypharmacology (Angew. Chem. Int. Ed. 30/2015)

Author(s) -

Frett Brendan,

Carlomagno Francesca,

Moccia Maria Luisa,

Brescia Annalisa,

Federico Giorgia,

De Falco Valentina,

Admire Brittany,

Chen Zhongzhu,

Qi Wenqing,

Santoro Massimo,

Li Hongyu

Publication year - 2015

Publication title -

angewandte chemie international edition

Language(s) - English

Resource type - Reports

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.201505540

Subject(s) - vegf receptors , int , kinase , cover (algebra) , dual (grammatical number) , chemistry , cancer research , pharmacology , medicine , biochemistry , computer science , philosophy , mechanical engineering , engineering , operating system , linguistics

The inhibitory powers of a next‐generation inhibitor were carefully balanced so that it is equally potent on the RET kinase and VEGFR 2 . In their Communication on page 8717 ff., H.‐y. Li, M. Santoro, et al. report the optimization of a dual inhibitor for the treatment of RET‐driven malignancies through synergistic medicinal chemistry. The inhibitor is capable of simultaneously treating the parenchyma (RET) and stroma (VEGFR 2 ) at the same therapeutic dose.

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